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Message: Useful review on epigenetics and CKD for the scientists

"we don't want a technology that is TOOOO new"

Mmmm... as Bear would say, somebody has been sleeping in class. The whole point of apabetalone is that it has a novel MOA. No BET inhibitor has been approved yet - hence RVX had (and potentially still has) the chance to have a 'first-in-class' drug in apabetalone.  Failing the phase III trial was a huge blow because there a number of Betis in clinical trials that now are back in the race.

Bear has listed other BETis in development a few times.  They are targeting cancer targets.  Notable among them are those that Abbvie is developing because they have BD2 specific molecules as well as panBET inhibitors.  And, as they say, these may have a good safety and tolerability profile:

"Together, these in vitro and in vivo results provide proof of concept that highly selective BDII BET family bromodomain inhibitors may have improved tolerability relative to pan-BET inhibitors while maintaining tumor growth inhibition in AML and AR positive prostate cancer."

https://cancerres.aacrjournals.org/content/78/13_Supplement/DDT01-05

Giddy-up RVX,

Jupe

 

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